322 receptor agonist function, namely (R)-(-)-3-[(R)-2-hydroxy-2-cyclopentyl-2-phenyl]ethoxy-1-{2-[4-((R)2-{(R)-[2-hydroxy-2-(3-formamido-4-hydroxy)phenyl]ethylamino}propyl)phenoxy]propyl}-1-azabicyclo[2,2,2]octylonium hydrochloride chloride, as well as crystallization and preparation methods therefor, and a use thereof. The compound can form a crystalline solid, has better stability and solubility in water, has a faster onset time for airway relaxation, and is more suitable for drug preparation.
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
A61K 31/49 - Dérivés du cinchonane, p. ex. quinine
Disclosed are a solution type nasal spray containing 3-[(2-cyclopentyl-2-hydroxy-2-phenyl)ethoxy]-1-(3-phenoxypropyl)-1-azabicyclo[2,2,2]octonium salt or a derivative thereof, and a preparation method therefor. The components of the solution-type nasal spray include an active pharmaceutical ingredient, a solvent, a cosolvent, a bacteriostatic agent, a pH regulator and an osmotic pressure regulator. The nasal spray has high stability; a pharmacodynamic test result shows that the nasal spray takes effect quickly and is less irritating, and can be used for treating different types of rhinitis and cold accompanied rhinitis.
A61K 31/49 - Dérivés du cinchonane, p. ex. quinine
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
A61P 11/02 - Agents rhinologiques, p. ex. décongestionnants
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
A61P 13/10 - Médicaments pour le traitement des troubles du système urinaire de la vessie
A61P 13/00 - Médicaments pour le traitement des troubles du système urinaire
A61P 13/02 - Médicaments pour le traitement des troubles du système urinaire de l'urine ou des voies urinaires, p. ex. acidificateurs d'urine
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
A61P 1/04 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des ulcères, des gastrites ou des œsophagites par reflux, p. ex. antiacides, antisécrétoires, protecteurs de la muqueuse
3.
Crystals, preparation method and application of a muscarinic receptor antagonist
The present invention provides crystals of a quaternary ammonium salt structure compound, i.e., (2R,3R)-3-[(2-cyclopentyl-2-hydroxy-2-phenyl)ethoxy]-1-(3-phenoxypropyl) azabicyclo[2,2,2]octylonium bromide (Compound I). A Type-A crystal of Compound I displays diffraction peaks at the following diffraction angles 2θ in a X-ray powder diffraction pattern thereof: 5.7±0.2 degrees, 12.9±0.2 degrees, 16.7±0.2 degrees, 18.0±0.2 degrees, 19.5±0.2 degrees, 21.1±0.2 degrees, 22.3±0.2 degrees and 23.3±0.2 degrees. A Type-B crystal of Compound I displays diffraction peaks at the following diffraction angles 2θ in a X-ray powder diffraction pattern thereof: 5.2±0.2 degrees, 15.8±0.2 degrees, 16.9±0.2 degrees, 17.7±0.2 degrees, 19.5±0.2 degrees, 20.2±0.2 degrees and 22.1±0.2 degrees. The present application also relates to a new method for preparing Compound I and applications of the two novel crystals in the field of medicine.
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
4.
CRYSTAL OF M RECEPTOR ANTAGONIST AS WELL AS PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
The main purpose of the present invention is to provide a novel crystal of a quaternary ammonium salt structure compound, i.e., (2R,3R)-3-[(2-cyclopentyl-2-hydroxy-2-phenyl)ethoxy]-1-(3-phenoxypropyl)-1-azabicyclo[2,2,2]octylonium bromide (hereinafter referred to as compound I). A type A crystal of compound I displays diffraction peaks at the following diffraction angles 2θ in a powder X-ray diffraction pattern thereof: 5.7±0.2 degrees, 12.9±0.2 degrees, 16.7±0.2 degrees, 18.0±0.2 degrees, 19.5±0.2 degrees, 21.1±0.2 degrees, 22.3±0.2 degrees and 23.3±0.2 degrees. A type B crystal of compound I displays diffraction peaks at the following diffraction angles 2θ in a powder X-ray diffraction pattern thereof: 5.2±0.2 degrees, 15.8±0.2 degrees, 16.9±0.2 degrees, 17.7±0.2 degrees, 19.5±0.2 degrees, 20.2±0.2 degrees and 22.1±0.2 degrees. The present invention also relates to a new preparation method for compound I and an application of the two novel crystals in the field of medicine.
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
A61K 31/49 - Dérivés du cinchonane, p. ex. quinine
A61P 11/02 - Agents rhinologiques, p. ex. décongestionnants
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
Provided is 2-(4-diethylamino)butylmalonic acid-(1R,2R)-(−)-1,2-cyclohexanediamine platinum(II) phosphate having high solubility, low hygroscopicity, and high stability and being suitable for preparing into various antitumor drug preparations. Also provided is a preparation method for amorphous 2-(4-diethylamino)butylmalonic acid-(1R,2R-)-1,2-cyclohexanediamine platinum(II) phosphate. The method is simple to operate and is suitable for industrial implementation.
Provided is 2-(4-diethylamino)butylmalonic acid-(1R,2R)-(-)-1,2-cyclohexanediamine platinum(II) phosphate having high solubility, low hygroscopicity, and high stability and being suitable for preparing into various antitumor drug preparations. Also provided is a preparation method for amorphous 2-(4-diethylamino)butylmalonic acid-(1R,2R)-(-)-1,2-cyclohexanediamine platinum(II) phosphate. The method is simple to operate and is suitable for industrial implementation.
2-adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and optical isomer thereof. A pharmaceutical composition comprising such a compound with quaternary ammonium salt structure, a method for preparing such a compound with quaternary ammonium salt structure and an intermediate thereof, and uses thereof in treating pulmonary disorders are also provided. The compounds of the invention have high selectivity to the M receptor subtype, and have less adverse reaction and lower toxic and side effects in the treatment of pulmonary diseases such as COPD and asthma.
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
Provided are a class of compounds, as represented by formula (I), having a bifunctional active quaternary ammonium salt structure of a β2 adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and an optical isomer thereof, and a pharmaceutical composition containing such a compound with the quaternary ammonium salt structure, a method for preparing such a compound with the quaternary ammonium salt structure and an intermediate thereof, and the use thereof in treating pulmonary diseases. The compound of the present invention has high selectivity for M receptor subtypes, and has the characteristics of fewer adverse effects and less toxic side effects in the treatment of pulmonary diseases such as COPD and asthma.
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
C07D 453/00 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine
2 receptor subtype, and the above compounds are characterized by rapid action, long-lasting efficacy, and low toxic and side-effects when used to treat rhinitis, post-cold rhinitis, chronic trachitis, airway hyperresponsiveness, asthma, chronic obstructive pulmonary diseases, cough, urinary incontinence, frequent urination, unstable bladder syndrome, bladder spasms, bladder inflammation and gastrointestinal diseases such as irritable bowel syndrome, spastic colitis, as well as duodenal and gastric ulcers.
A61K 31/46 - Aza-8-bicyclo[3.2.1]octaneSes dérivés, p. ex. atropine, cocaïne
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/439 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle le cycle formant une partie d'un système cyclique ponté, p. ex. quinuclidine
10.
Platinum compounds of malonic acid derivative having leaving group containing amino or alkylamino
Disclosed are a class of platinum compounds of malonic acid derivatives having a leaving group containing an amino or alkylamino, and pharmaceutically acceptable salt thereof, preparation method thereof and pharmaceutical composition containing the compounds. Also disclosed are uses of the compounds for treating cell proliferative diseases especially cancers. The platinum compounds of the present invention have high solubility in water, low toxicity and strong anti-tumor effect.
Disclosed are a category of platinum compounds having amino- or alkylamino-containing succinato derivatives as leaving group, or pharmaceutically acceptable salts thereof, preparation method thereof, and medicinal compositions containing the compounds. Also disclosed is a use of the compounds in treating cell proliferative diseases, especially cancers. The platinum compounds of the present invention have high water solubility and small toxic side effect.
A61K 31/555 - Composés hétérocycliques contenant des métaux lourds, p. ex. hémine, hématine, mélarsoprol
C07C 67/343 - Préparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone
C07C 227/04 - Formation de groupes amino dans des composés contenant des groupes carboxyle
C07C 227/18 - Préparation de composés contenant des groupes amino et carboxyle liés au même squelette carboné à partir de composés contenant déjà des groupes amino et carboxyle ou leurs dérivés par des réactions impliquant des groupes amino ou carboxyle, p. ex. hydrolyse d'esters ou d'amides, par formation d'halogénures, de sels ou d'esters
C07D 295/15 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes d'azote du cycle substitués par des atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile avec les atomes d'azote du cycle et les atomes de carbone comportant trois liaisons à des hétéro-atomes liés à la même chaîne carbonée, qui n'est pas interrompue par des carbocycles à une chaîne acyclique saturée
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
12.
Platinum compounds for treating cell proliferative diseases, preparation method and use thereof
Disclosed are a class of platinum compounds with a leaving group of malonic acid derivatives containing amino and alkylamino, their pharmaceutically acceptable salts, their preparation methods and pharmaceutical composites comprising them. Disclosed also are for the uses of the compounds in the treatment of cell proliferative diseases, particularly for the treatment of cancers. The present platinum compounds have high water solubility and low toxicity.
A61K 31/351 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle non condensés avec un autre cycle
13.
CLASS OF BIFUNCTIONAL COMPOUNDS WITH QUATERNARY AMMONIUM SALT STRUCTURE
Provided are a class of compounds, as represented by formula (I), having a bifunctional active quaternary ammonium salt structure of a ß2 adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and an optical isomer thereof, and a pharmaceutical composition containing such a compound with the quaternary ammonium salt structure, a method for preparing such a compound with the quaternary ammonium salt structure and an intermediate thereof, and the use thereof in treating pulmonary diseases. The compound of the present invention has high selectivity for M receptor subtypes, and has the characteristics of fewer adverse effects and less toxic side effects in the treatment of pulmonary diseases such as COPD and asthma.
A61K 31/439 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle le cycle formant une partie d'un système cyclique ponté, p. ex. quinuclidine
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
A61K 31/538 - 1,4-Oxazines, p. ex. morpholine condensées en ortho ou en péri avec des systèmes carbocycliques
C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
14.
PHOSPHATE OF PLATINUM COMPOUND AND PREPARATION METHOD THEREFOR
The present invention belongs to the field of medical technology. In particular, provided is 2-(4- diethylamino)butylmalonic acid-(lR,2R)-(-)-l,2-cyclohexanediamine platinum(II) phosphate of Formula (1) having high solubility, low hygroscopicity, and high stability and being suitable for preparing into various antitumor drug preparations. Also provided is a preparation method for amorphous 2-(4-diethylamino)butylmalonic acid-(lR,2R)-(-)-l,2- cyclohexanediamine platinum(II) phosphate. The method is simple to operate and is suitable for industrial implementation.
The main purpose of the present invention is to provide a novel crystal of a quaternary ammonium salt structure compound, i.e., (2R,3R)-3-[(2-cyclopentyl-2-hydroxy-2-phenyl)ethoxy]-1-(3-phenoxypropyl)-1-azabicyclo[2,2,2]octylonium bromide (hereinafter referred to as compound I). A type A crystal of compound I displays diffraction peaks at the following diffraction angles 2? in a powder X-ray diffraction pattern thereof: 5.7±0.2 degrees, 12.9±0.2 degrees, 16.7±0.2 degrees, 18.0±0.2 degrees, 19.5±0.2 degrees, 21.1±0.2 degrees, 22.3±0.2 degrees and 23.3±0.2 degrees. A type B crystal of compound I displays diffraction peaks at the following diffraction angles 2? in a powder X-ray diffraction pattern thereof: 5.2±0.2 degrees, 15.8±0.2 degrees, 16.9±0.2 degrees, 17.7±0.2 degrees, 19.5±0.2 degrees, 20.2±0.2 degrees and 22.1±0.2 degrees. The present invention also relates to a new preparation method for compound I and an application of the two novel crystals in the field of medicine.
A61P 13/10 - Médicaments pour le traitement des troubles du système urinaire de la vessie
C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p. ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
brevets
